5-Cyclic Amine-3-arylsulfonylindazoles as Novel 5-HT6 Receptor Antagonists

被引：20
|
作者：
Haydar, Simon N. [1 ]
Yun, Heedong [1 ]
Andrae, Patrick M. [1 ]
Mattes, James [1 ]
Zhang, Jean [2 ]
Kramer, Angela [2 ]
Smith, Deborah L. [2 ]
Huselton, Christine [3 ]
Graf, Radka [2 ]
Aschmies, Suzan [2 ]
Schechter, Lee E. [2 ]
Comery, Thomas A. [2 ]
Robichaud, Albert J. [1 ]
机构：
[1] Wyeth Ayerst Res, Chem Sci, Princeton, NJ 08543 USA
[2] Wyeth Ayerst Res, Discovery Neurosci, Princeton, NJ 08543 USA
[3] Wyeth Ayerst Res, Drug Safety & Metab, Collegeville, PA 19426 USA
来源：
JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 53卷 / 06期
关键词：
ACETYLCHOLINE-RELEASE; POTENT; DERIVATIVES; LOCALIZATION; DISCOVERY; SB-271046; HYDROGEN; LIGANDS; CORTEX;
D O I：
10.1021/jm901674f
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
Novel 5-cyclic amine-3-arylsulfonylindazoles were prepared, and several analogues within this class have been identified as high-affinity 5-HT6 receptor ligands with improved pharmacokinetic and pharmacological properties. One selected example, 18b, showed good brain penetrability and a generally favorable pharmacokinetic profile with procognitive efficacy in the rat novel object recognition assay. The synthesis and structure activity relationship of this potent class are discussed.
引用
收藏
页码：2521 / 2527
页数：7
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